Das pharmakologische Profil von Sildenafil zeigt neben der PDE5-Inhibition auch eine geringe Aktivität an der PDE6 in der Retina. Dies erklärt visuelle Nebenwirkungen wie Farbsehstörungen, die gelegentlich auftreten. Die orale Bioverfügbarkeit beträgt etwa 40 %, mit einer hohen Bindung an Plasmaproteine. Das Verteilungsvolumen ist groß, sodass die Substanz rasch in verschiedene Gewebe gelangt. Die Metabolisierung erfolgt hepatisch und produziert einen aktiven Metaboliten, der die pharmakologische Wirkung ergänzt. Nebenwirkungen sind dosisabhängig und umfassen Kopfschmerzen, Hautrötung und Dyspepsie. Bei Vergleichen innerhalb der Wirkstoffklasse wird viagra original regelmäßig als Beispiel für eine Substanz mit schneller, aber kurzzeitiger Wirkung aufgeführt.

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